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New semi-synthetic analogs of oleuropein show improved anticancer activity in?vitro and in?vivo

Oleuropein is a glucosylated seco-iridoid present in olive fruits and leaves. Due to its broad spectrum of biological activities, including anticancer properties, oleuropein has attracted scientific attention for the past 20 years. The promising antiproliferative activity of an olive leaf extract enriched in oleuropein against a series of human cancer cell lines, prompted us to proceed with the semi-synthesis of 51 analogs of oleuropein. Following their initial screening against the estrogen receptor negative breast cancer cell line SKBR3, 7 analogs were shown to display significant cytotoxicity and were further tested against 6 additional solid tumor-derived and leukemic cell lines. The analog with the most promising antitumor activity (24) was selected for more detailed studies. 24 was non-toxic to peripheral blood mononuclear cells derived from healthy blood donors when tested at concentrations close to its half maximal inhibitory concentration. In vivo administration of 24 in melanoma-bearing mice resulted in reducing tumor size in a dose-dependent manner and in inducing anti-melanoma-reactive immune responses. Our results suggest that analog 24, emerging from the initial structure of oleuropein, represents a promising lead structure for further optimization.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Awesome and Easy Science Experiments about Ethyl 2,3-dihydrobenzo[1,4]dioxine-2-carboxylate

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SELECTIVE INHIBITORS OF NLRP3 INFLAMMASOME

The present disclosure relates to compounds of Formula (I): (I); and to their pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein are useful for inhibiting the maturation of cytokines of the IL-1 family by inhibiting inflammasomes and may be used in the treatment of disorders in which inflammasome activity is implicated, such as autoinflammatory and autoimmune diseases and cancers.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

More research is needed about 22013-33-8

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Novel azanaphtoquinone compounds with aromatic amino moiety: Synthesis, structural characterization, and antimicrobial features

New azanaphtoquinone compounds with aromatic moiety were synthesized and their structures were defined by Fourier transform infrared, 13C NMR, 1H NMR and mass spectra. The activities of synthesized azanaphthoquinones as antimicrobial agents against three strains of Gram-positive, four strains of Gram-negative and as well as against three strains of fungi were also investigated. Compound 3d showed eight times greater antibacterial activity against the most sensitive organism being S. epidermidis with a MIC value of 1.22 mug/mL than the reference antimicrobial compound Cefuroxime (MIC = 9.8 mug/mL). For compound 3c, the antibacterial activity against S. epidermidis and S. aureus was equal to that of Cefuroxime and Cefuroxime-Na, respectively. The antibacterial activity of the compounds 3c and 3d were two times stronger against E. faecalis than the reference antimicrobial compound Amikacin. The results obtained in this study revealed that newly synthesized compounds 3c, 3d, and 3e are effective in treating infectious caused by especially Gram-positive bacteria have developed multiple resistances to antibiotics and are favorable structures in designing novel antimicrobial agents.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Reference of 214894-89-0, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 214894-89-0, molcular formula is C9H9BrO2, introducing its new discovery.

2-ALKYL-INDAZOLE COMPOUNDS FOR THE TREATMENT OF CERTAIN CNS-RELATED DISORDERS

2-Alkyl-indazole compound and its pharmaceutically acceptable salts of acid addition, method and intermediates for preparing them, a pharmaceutical composition containing them and use of the latter. The 2-alkyl-indazole compound has the following general formula (I) in which R1, R2, R3, R4, R6, R7, X, Y, W, n, p, and m have the meanings stated in the description.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Some scientific research about 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine

The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 22013-33-8 is helpful to your research. Synthetic Route of 22013-33-8

Synthetic Route of 22013-33-8, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 22013-33-8, molcular formula is C8H9NO2, introducing its new discovery.

1,2,3-Dithiazoles-new reversible melanin synthesis inhibitors: A chemical genomics study

A chemical genomic screen of an in-house library of small molecule heterocycles was carried out using Xenopus laevis embryos. This led to the identification of N-(4-chloro-5H-1,2,3-dithiazol-5-ylidene)-4-methoxyaniline (1c), which elicits loss of pigmentation in melanophores and the retinal pigment epithelium (RPE) of developing embryos, independent of the developmental stage of initial exposure. The phenotype was reversible, since pigmentation returned upon compound removal while analysis of neural crest cell markers (Pax7) and melanophore markers (Dct/Xtrp2) revealed that both neural crest precursors and fully differentiated melanophores were present in the dithiazole 1c treated embryos. A subsequent focused structure-activity relationship (SAR) study identified the more active dithiazole 4-benzyloxy-N-(4-chloro-5H-1,2,3-dithiazol-5-ylidene)-aniline (1l) and the need for a chlorine substituent at the dithiazole C-4 position. Both the initial chemical genomic screen and the focused SAR study highlighted the toxicity of (dithiazolylidene)aminoazines, and also of methoxyaniline (anisidine) analogues that hosted strong electron-withdrawing or electronegative substituents or acidic hydroxyl groups on the anisidine moiety. This study suggests that 1,2,3-dithiazoles can act as reversible melanin synthesis inhibitors, revealing a new biological activity for this class of compounds. The inhibition of melanin synthesis is medically relevant as a potential treatment for pigmentation disorders such as melasma.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

The Absolute Best Science Experiment for 6-Hydroxy-1,4-benzodioxane

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Synthesis of annulated dioxins as electron-rich donors for cation radical salts

The synthesis of a series of new alkoxylated linearly annulated dioxins is described together with their cyclic voltammetric behavior and some preliminary result on their ability to form cation radical salts. Of these dioxins, seven (8, 12, 19, 21, 27, 33, 34) are the first representatives of entirely new heterocyclic systems. Dioxins 8, 21, 22 and 27 gave good quality cation radical salts upon electrocrystallization. Graphical Abstract

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Archives for Chemistry Experiments of 2,3-Dihydrobenzo[b][1,4]dioxine-5-carboxylic acid

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Electric Literature of 4442-53-9, Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Patent, and a compound is mentioned, 4442-53-9, 2,3-Dihydrobenzo[b][1,4]dioxine-5-carboxylic acid, introducing its new discovery.

SWEET FLAVOR MODIFIER

The present invention includes compounds having structural formula (I), or pharmaceutically acceptable salts, solvate, and/or ester thereof. These compounds are useful as sweet flavor modifiers. The present invention also includes compositions comprising the present compounds and methods of enhancing the sweet taste of ingestible compositions. Furthermore, the present invention provides methods for preparing the compounds.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Some scientific research about 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine

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Related Products of 22013-33-8, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.22013-33-8, Name is 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine, molecular formula is C8H9NO2. In a Article£¬once mentioned of 22013-33-8

Multi-dimensional target profiling of N,4-diaryl-1,3-thiazole-2-amines as potent inhibitors of eicosanoid metabolism

Eicosanoids like leukotrienes and prostaglandins play a considerable role in inflammation. Produced within the arachidonic acid (AA) cascade, these lipid mediators are involved in the pathogenesis of pain as well as acute and chronic inflammatory diseases like rheumatoid arthritis and asthma. With regard to the lipid cross-talk within the AA pathway, a promising approach for an effective anti-inflammatory therapy is the development of inhibitors targeting more than one enzyme of this cascade. Within this study, thirty N-4-diaryl-1,3-thiazole-2- amine based compounds with different substitution patterns were synthesized and tested in various cell-based assays to investigate their activity and selectivity profile concerning five key enzymes involved in eicosanoid metabolism (5-, 12-, 15-lipoxygenase (LO), cyclooxygenase-1 and -2 (COX-1/-2)). With compound 7, 2-(4-phenyl)thiazol-2-ylamino)phenol (ST-1355), a multi-target ligand targeting all tested enzymes is presented, whereas compound 9, 2-(4-(4-chlorophenyl)thiazol-2-ylamino)phenol (ST-1705), represents a potent and selective 5-LO and COX-2 inhibitor with an IC50 value of 0.9 ¡À 0.2 muM (5-LO) and a residual activity of 9.1 ¡À 1.1% at 10 muM (COX-2 product formation). The promising characteristics and the additional non-cytotoxic profile of both compounds reveal new lead structures for the treatment of eicosanoid-mediated diseases.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Archives for Chemistry Experiments of 1-(2,3-Dihydrobenzo[b][1,4]dioxin-6-yl)ethanone

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Electric Literature of 2879-20-1, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 2879-20-1, molcular formula is C10H10O3, introducing its new discovery.

Rhodium-Catalyzed Oxidative Cycloaddition of N-tert-Butoxycarbonylhydrazones with Alkynes for the Synthesis of Functionalized Pyrroles via C(sp3)?H Bond Functionalization

A rhodium(III)-catalyzed cycloaddition of N-tert-butoxycarbonylhydrazones with internal alkynes was developed. The reaction features a regioselective alpha-imino alkyl C(sp3)?H bond functionalization resulting in selective formation of highly functionalized NH-free pyrroles. Our studies showed that utilizing the N-tert-butoxycarbonyl (N-Boc) as the oxidizing directing group is critical for achieving the observed pyrrole formation versus the isoquinoline formation. To account for the pyrrole formation, we hypothesized that a prior tautomerization of the N-Boc-hydrazones to enamines should occur, followed by regioselective C(sp2)?H cleavage to form a putative five-membered rhodacycle. Subsequent coupling of the rhodacycle with the alkynes would afford the pyrrole products. (Figure presented.).

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Palladium-catalyzed selective synthesis of 3,4-dihydroquinazolines from electron-rich arylamines, electron-poor arylamines and glyoxalates

A simple palladium-catalyzed selective synthesis of structurally diverse 3,4-dihydroquinazolines from electron-rich arylamines, electron-poor arylamines and glyoxalates has been developed under mild conditions. This reaction is carried out in a tandem manner constituted by the condensation of arylamines and glyoxalates, the selective Diels-Alder cycloaddition and oxidation processes, in which 4-nitrothiophenol was used as the key ligand.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem